Abstract:
:A series of 2-aryldopamine analogues were synthesized and evaluated for their effects on D1 and D2 dopamine receptors. The 2-phenyldopamine and 6-phenylbenzazepine analogues exhibited weak binding to both D1 and D2 receptors. The 9-(aminomethyl)fluorenes also exhibited weak D2 binding; however, 2,5,6-trihydroxy-9H-fluorene-9-methanamine (4b) exhibited D1 binding comparable to apomorphine. The binding activity has been correlated with the calculated torsion angle of the biphenyl portion of these molecules. Good D1 dopamine binding occurs when the aromatic rings approach coplanarity; poor binding occurs when the aromatic rings are orthogonal.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Ladd DL,Weinstock J,Wise M,Gessner GW,Sawyer JL,Flaim KEdoi
10.1021/jm00160a018subject
Has Abstractpub_date
1986-10-01 00:00:00pages
1904-12issue
10eissn
0022-2623issn
1520-4804journal_volume
29pub_type
杂志文章abstract::This paper describes the synthesis and pharmacological evaluation of a number evaluation of a number of substituted 1,3,4-thiadiazoles. The first member of the series, 2-(aminomethyl)-5-(2-biphenylyl)-1,3,4-thiadiazole (7) was found to possess potent anticonvulsant properties in rats and mice and compared favorably wi...
journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
doi:10.1021/jm00161a025
更新日期:1986-11-01 00:00:00
abstract::Detailed molecular models of the free C1B domain of protein kinase C-gamma (PKC-gamma) and the C1B domain with its activator phorbol-12-myristate-13-acetate (PMA) in water solution and in the presence of dipalmitoylphosphatidylcholine (DPPC) bilayer are presented. Molecular dynamics of the free C1B domain reveals hydr...
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章
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journal_title:Journal of medicinal chemistry
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更新日期:2013-04-11 00:00:00
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journal_title:Journal of medicinal chemistry
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